ArticleSpringerPlus2016
Synthesis, anti-inflammatory, bactericidal activities and docking studies of novel 1,2,3-triazoles derived from ibuprofen using click chemistry.
Article in SpringerPlus, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 91 citations in OpenAlex.
- Study on Synthesis, Antiproliferative Properties, Immunomodulatory Effects, and Anti-Breast Cancer Activity of New ΔChemistry & biodiversity · 2026Article
- Structural Modifications of Nonsteroidal Anti-Inflammatory Drugs (NSAIDs): New Horizons in Antimicrobial Drug Discovery.Archiv der Pharmazie · 2026Review
- α-Glycosidase activity of novel coumarin-triazole-coumarin dyads.Turkish journal of chemistry · 2025Article
- Design, synthesis, analgesic, antibacterial and docking studies of novel 8-piperazinylcaffeine carboxylate ionic liquids.RSC advances · 2024Article
- New Diaryl-1,2,4-triazolo[3,4-ACS omega · 2024Article
- Design, synthesis, and cytotoxicity of ibuprofen-appended benzoxazole analogues against human breast adenocarcinoma.RSC medicinal chemistry · 2024Article
- Cholinesterase Inhibitory and Anti-Inflammatory Activity of the Naphtho- and Thienobenzo-Triazole Photoproducts: Experimental and Computational Study.International journal of molecular sciences · 2023Article
- Towards Anticancer and Antibacterial Agents: Design and Synthesis of 1,2,3-Triazol-quinobenzothiazine Derivatives.International journal of molecular sciences · 2023Article
- Meldrum-Based-1ACS omega · 2023Article
- Fungicide sensitivity of grapevine bacteria with plant growth-promoting traits and antagonistic activity as non-target microorganisms.World journal of microbiology & biotechnology · 2023Article
- Discovery of New Boswellic Acid Hybrid 1Pharmaceuticals (Basel, Switzerland) · 2023Article
- Recent Advances in Bioactive Flavonoid Hybrids Linked by 1,2,3-Triazole Ring Obtained by Click Chemistry.Molecules (Basel, Switzerland) · 2021Review
- Application of triazoles in the structural modification of natural products.Journal of enzyme inhibition and medicinal chemistry · 2021Review
- CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review.RSC advances · 2020Review
- Article
- Ibuprofen-Loaded Hyaluronic Acid Nanofibrous Membranes for Prevention of Postoperative Tendon Adhesion through Reduction of Inflammation.International journal of molecular sciences · 2019Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundNonsteroidal anti-inflammatory drugs are of vast therapeutic benefit in the treatment of different types of inflammatory conditions. 1,2,3-Triazoles and their derivatives have a wide range of applications as anti-bacterial, anti-fungal, anti-tubercular, cytostatic, anti-HIV, anti-allergic, anti-neoplastic and anti-inflammatory (AI) agents. Considering the individual biological and medicinal importance of ibuprofen and 1,2,3-triazoles, we wanted to explore novel chemical entities based on ibuprofen and triazole moieties towards their biological significance.
resultsClick chemistry has utilized as an ideal strategy to prepare novel ibuprofen-based 1,4-disubstituted 1,2,3-triazole containing molecules. These compounds were screened for their in vivo AI activity, among all the synthesized analogues 13o was shown potent effect than the reference AI drug ibuprofen at the same concentration (10 mg/kg body weight). Compounds 13l, 13g, 13c, 13k, 13i, 13n, 13m and 13j were shown significant AI activity. These triazole analogues were also screened for their bactericidal profile. Compounds 13c, 13i, 13l and 13o exhibited considerable bactericidal activity against gram positive and gram negative strains. In addition to this, molecular docking studies were also carried out into cyclooxygenase-2 active site to predict the affinity and orientation of these novel compounds (13a-q).
conclusionsIn summary, we have designed and synthesized 1,2,3-triazole analogues of ibuprofen in good yields using Click chemistry approach. AI and bactericidal activities of these compounds were evaluated and shown remarkable results.
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